Fusicoccane Diterpenes from Hypoestes forsskaolii as Heat Shock Protein 90 (Hsp90) Modulators

被引：24

作者：

D'Ambola, Massimiliano ^{[1
]}

Fiengo, Lorenzo ^{[1
]}

Chini, Maria Giovanna ^{[1
]}

Cotugno, Roberta ^{[1
]}

Bader, Ammar ^{[3
]}

Bifulco, Giuseppe ^{[1
]}

Braca, Alessandra ^{[4
,5
]}

De Tommasi, Nunziatina ^{[1
]}

Dal Piaz, Fabrizio ^{[1
,2
]}

机构：

[1] Univ Salerno, Dipartimento Farm, Via Giovanni Paolo II 132, I-84084 Fisciano, SA, Italy

[2] Univ Salerno, Dipartimento Med Chirurg & Odontoiatria Scuola Me, Via Giovanni Paolo II 132, I-84084 Fisciano, SA, Italy

[3] Umm Al Qura Univ, Dept Pharmacognosy, Fac Pharm, Mecca 21955, Saudi Arabia

[4] Univ Pisa, Dipartimento Farm, Via Bonanno 33, I-56126 Pisa, Italy

[5] Univ Pisa, Ctr Interdipartimentale Ric Nutraceut & Alimentaz, Via Borghetto 80, I-56124 Pisa, Italy

来源：

JOURNAL OF NATURAL PRODUCTS | 2019年 / 82卷 / 03期

关键词：

INHIBITORS;

D O I：

10.1021/acs.jnatprod.8b00924

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

Ten new (1-10) and six known (11-16) fusicoccane diterpenes were isolated from the roots of Hypoestes forsskaolii. The structural characterization of 1-10 was performed by spectroscopic analysis, including 1D and 2D NMR, ECD, and HRESIMS experiments. From a perspective of obtaining potential Hsp90a inhibitors, the isolates were screened by surface plasmon resonance measurements and their cytotoxic activity was assayed using Jurkat and HeLa cancer cells. Compound 6, 18-hydroxyhypoestenone, was shown to be the most active compound against Hsp90, and its interactions were studied also by biochemical and cellular assays and by molecular docking.

引用

页码：539 / 549

页数：11

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